Abstract

A system of novel nanoparticles of star-shaped cholic acid-core polylactide-D-α-tocopheryl polyethylene glycol 1000 succinate (CA-PLA-TPGS) block copolymer was
developed for paclitaxel delivery for breast cancer treatment, which demonstrated
superior in vitro and in vivo performance in comparison with paclitaxel-loaded poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles and linear PLA-TPGS nanoparticles. The paclitaxel-
or couramin 6-loaded nanoparticles were fabricated by a modified nanoprecipitation
method and then characterized in terms of size, surface charge, surface morphology,
drug encapsulation efficiency, and in vitro drug release. The CA-PLA-TPGS nanoparticles were found to be spherical in shape with
an average size of around 120 nm. The nanoparticles were found to be stable, showing
no change in the particle size and surface charge during 90-day storage of the aqueous
solution. The release profiles of the paclitaxel-loaded nanoparticles exhibited typically
biphasic release patterns. The results also showed that the CA-PLA-TPGS nanoparticles
have higher antitumor efficacy than the PLA-TPGS nanoparticles and PLGA nanoparticles
in vitro and in vivo. In conclusion, such nanoparticles of star-shaped cholic acid-core PLA-TPGS block
copolymer could be considered as a potentially promising and effective strategy for
breast cancer treatment.